1. Stem Cell/Wnt
  2. β-catenin
  3. Tegatrabetan

Tegatrabetan (Synonyms: BC2059)

Cat. No.: HY-109103
Handling Instructions

Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1).

For research use only. We do not sell to patients.

Tegatrabetan Chemical Structure

Tegatrabetan Chemical Structure

CAS No. : 1227637-23-1

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Description

Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1)[1].

IC50 & Target

β-Catenin[1]

In Vitro

Tegatrabetan (BC2059; 20-100 nM; 48 hours) inhibits cell proliferation in suspension culture over 120 hours and induces apoptosis of cultured human acute myeloid leukemia (AML) HL-60, OCI-AML3 and MV4-11 cells dose-dependently[1].
Tegatrabetan (20 and 50 nM; 24 hours) induces a modest but significant accumulation of cells in the G0/G1 phase, with a concomitant decline in the G2/M phase of the cell cycle[1].
Tegatrabetan (100 nM, 24 hours) depletes the levels of β-catenin and its target genes, including c-MYC and survivin without affecting the levels of the TBL1 in OCI-AML3, HL-60 and MV4-11 cells[1].

Cell Proliferation Assay[1]

Cell Line: HL-60, OCI-AML3 and MV4-11 cells
Concentration: 20, 50, and 100 nM
Incubation Time: 48 hours
Result: Dose-dependently inhibited cell proliferation.

Cell Cycle Analysis[1]

Cell Line: OCI-AML3 cells
Concentration: 20 and 50 nM
Incubation Time: 24 hours
Result: Dose-dependently induced cell cycle growth arrest.

Western Blot Analysis[1]

Cell Line: OCI-AML3, HL-60 and MV4-11 cells
Concentration: 100 nM
Incubation Time: 24 hours
Result: Treatment depleted β-Catenin expression levels.
In Vivo

Tegatrabetan (BC2059; 1.0 or 5.0 mg/kg/day; intravenously) significantly improves the median survival of the mice from approximately 17.5 to 39 days. Treatment with Tegatrabetan (10 mg/kg/day; intravenously) alone further improves the median survival to 51.5 days[1].

Animal Model: NOD/SCID mice bearing OCI-AML3 xenografts[1]
Dosage: 1 mg/kg; 5 mg/kg; 10 mg/kg
Administration: Intravenously; 1 mg/kg daily 4 days per week or 5 mg/kg or 10 mg/kg of BC2059 twice per week (Tuesday and Thursday) for 3 weeks.
Result: Treatment significantly improved survival of NOD/SCID mice bearing OCI-AML3 xenografts.
Molecular Weight

588.74

Formula

C₂₈H₃₆N₄O₆S₂

CAS No.

1227637-23-1

SMILES

O=S(C1=CC2=C(C=C1)/C(C3=CC=C(S(=O)(N4C[[email protected]](C)C[[email protected]](C)C4)=O)C=C3/C2=N\O)=N\O)(N5C[[email protected]](C)C[[email protected]](C)C5)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

TegatrabetanBC2059BC 2059BC-2059β-cateninBeta cateninInhibitorinhibitorinhibit

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